EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. By engaging with allosteric C111 in the E2 ubiquitin ligase UBE2D, EN450 facilitates the formation of a ternary complex involving UBE2D and NFKB1. This interaction leads to the degradation of NF-κB, resulting in notable anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism. EN450 serves as a valuable tool for research involving NF-κB signaling and its implications in cancer biology.
EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. By engaging with allosteric C111 in the E2 ubiquitin ligase UBE2D, EN450 facilitates the formation of a ternary complex involving UBE2D and NFKB1. This interaction leads to the degradation of NF-κB, resulting in notable anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism. EN450 serves as a valuable tool for research involving NF-κB signaling and its implications in cancer biology.
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